684286-88-2Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of novel tricyclic HIV-1 integrase inhibitors by modification of its pyridine ring
Metobo, Sammy E.,Jin, Haolun,Tsiang, Manuel,Kim, Choung U.
, p. 3985 - 3988 (2007/10/03)
This communication details both the syntheses and biological evaluation of a novel class of HIV-1 integrase inhibitors. When the quinoline moiety is replaced with the quinoxoline moiety, the antiviral activity is significantly compromised. Similarly, intr
Design and optimization of tricyclic phtalimide analogues as novel inhibitors of HIV-1 integrase
Verschueren, Wim G.,Dierynck, Inge,Amssoms, Katie I. E.,Hu, Lili,Boonants, Paul M. J. G.,Pille, Geert M. E.,Daeyaert, Frits F. D.,Hertogs, Kurt,Surleraux, Dominique L. N. G.,Wigerinck, Piet B. T. P.
, p. 1930 - 1940 (2007/10/03)
Human immunodeficiency virus type-1 integrase is an essential enzyme for effective viral replication and hence a valid target for the design of inhibitors. We report here on the design and synthesis of a novel series of phthalimide analogues as integrase
PHOSPHONATE ANALOGS OF HIV INTEGRASE INHIBITOR COMPOUNDS
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Page/Page column 534-535, (2010/02/15)
Novel HIV integrase inhibitor compounds having at least one phosphonate group, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.
HIV INTEGRASE INHIBITORS
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Page 51, (2010/02/09)
The present invention concerns the compounds having the formula (1), N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof wherein (a) or (b); A, together with the two carbons of the phenyl ring to which it is attached forms a monocyclic aryl or a monocyclic Het2 ; R1 is hydrogen, halo, nitro, cyano, sultam, sulltim, C3-7cycloalkyl, C(=O)-R5, S(=O)y-R6, OR 7, NR8R9, C(=NR8)-R5, optionally polysubstituted C1-6alkyl, optionally polysubstituted C2-6alkenyl or optionally polysubstituted C2-6alkynyl; R 2 is hydrogen, C3-7cycloalkyl, aryl, Het1, Het2, C(=O)-R5, S(=O)Y-R6 OR7, NR8R9, C=NR8)-R5, or optionally polysubstituted C1-6alkyl, optionally polysubstituted C2-6alkenyl or optionally polysubstituted C2-6alkynyl. It further relates to their use as HIV integrase inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with other anti-retroviral agents, and to their use in assays as reference compounds or as reagents.
PRE-ORGANIZED TRICYCLIC INTEGRASE INHIBITOR COMPOUNDS
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Page 295;296, (2008/06/13)
Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed. Formula (I). Al and A2 are moieties forming a five, six, or seven membered ring. L is a bond or a linker connecting a ring atom of Ar to N. X is O, S, or substituted nitrogen. Ar is aryl or heteroaryl. Q is N, +NR, or CR4. The aryl carbons may be independently substituted with substituents other than hydrogen. The compounds may include prodrug moieties covalently attached at any site.
